Composition as auxiliary means for oral medication

ABSTRACT

Compositions, specifically a jelly, are provided the use of which composition as an auxiliary means eases the taking of oral medication in solid form, which composition comprises iota-carrageenan as a jellifying agent and citric acid as a salivating agent, characterized in that the composition further comprises maltodextrin. In another aspect, the composition comprises a calcium sequestrant for adjusting Ca-ion activity of the composition. In one embodiment, the composition comprises iota-carrageenan in 0.7-1.0% in mass, citric acid in 0.06-0.07% in mass, maltodextrin in 1.5% in mass, all relative to the total mass of the composition, and an amount of a calcium sequestrant such that the Ca-ion activity of the composition is between 20 ppm and 80 ppm.

CROSS-REFERENCE TO RELATED APPLICATIONS

This application is a divisional of U.S. application Ser. No. 16/243,857(now U.S. Pat. No. XX,XXX,XXX), which in turn is a divisional of U.S.application Ser. No. 14/782,008 filed on Apr. 2, 2014 (now abandoned),which is the U.S. national phase of International Application No.PCT/NL2014/050199 filed 2 Apr. 2014, which designated the U.S. andclaims priority to NL Patent Application No. 2010552 filed 2 Apr. 2013,the entire contents of each of which are hereby incorporated byreference.

FIELD OF THE INVENTION

The present invention relates to the technical field of taking oralmedication. The present invention relates to a composition, specificallya jelly, the use of which is to ease the taking of oral medication insolid form, and to the use of such a composition as an auxiliary meansfor the stated purpose.

BACKGROUND OF THE INVENTION

Some people, inter alia young children and elderly people, experienceswallowing problems when taking oral medication. This problem may becaused by certain conditions such as dysphagia and/or xerostomia (hyposalivation, dry mouth), and it can also have a psycho-somatic cause,e.g. a physiological abnormality, or disgust regarding the size or tasteof the capsules or pills to be swallowed.

Several compositions according to the pre-amble are known from the priorart. The following relate to the use of a jelly or jelly-likecomposition to enhance swallowing and ingestion of solid medication. Oneknown composition that facilitates swallowing comprises a mixture ofmodified pre-gelatinized starch, a sugar alcohol and a water-solublefood fiber. Another known composition comprises a combination of twopolysaccharides and a xanthan gum and/or a carrageenan to improve thefunction of ingestion/swallowing. Yet another known compositioncomprises a coating for a medication, the coating comprising alubricating jelly that comprises gelatin and hydroxypropylmethylcellulose. Yet another known composition comprisesiota-carrageenan as a jellifying agent and citric acid as a salivatingagent.

All presently known compositions, specifically jellies, the use of whichis to ease the taking of oral medication in solid form, and to the useof such compositions as auxiliary means for the stated purpose, havetheir own disadvantages. One known composition is limited to mixing itwith medication in powder form only. The use of another knowncomposition provides an unstable suspension upon mixing with theintended medication. Yet another known composition has to be preparedeach and every time for every active standard and every dosage of theactive substance of the medication.

An object of the present invention is to provide an alternativecomposition, specifically a jelly, the use of which composition is as anauxiliary means to ease the taking of oral medication in solid form,which composition comprises iota-carrageenan as a jellifying agent andcitric acid as a salivating agent.

It is another object of the present invention to provide an alternativecomposition, specifically a jelly, the use of which composition is as anauxiliary means to ease the taking of oral medication in solid form,which composition comprises iota-carrageenan as a jellifying agent andcitric acid as a salivating agent, which composition can be mixed withoral medication in all known solid forms including pills, capsules,tablets and powders.

It is a further object of the invention to provide an alternativecomposition, specifically a jelly, the use of which composition as anauxiliary means is to ease the taking of oral medication in solid form,which composition comprises iota-carrageenan as a jellifying agent andcitric acid as a salivating agent, which composition upon mixing withoral medication can provide a stable suspension that can be swallowed oringested.

It is a further object of the invention to provide an alternativecomposition, specifically a jelly, the use of which composition as anauxiliary means is to ease the taking of oral medication in solid form,which composition comprises iota-carrageenan as a jellifying agent andcitric acid as a salivating agent, which composition does not require tobe prepared for every active standard and every dosage of the activesubstance of the oral medication to be swallowed.

It is yet another object of the present invention to provide analternative composition, specifically a jelly, the use of whichcomposition as an auxiliary means is to ease the taking of oralmedication in solid form, which composition comprises iota-carrageenanas a jellifying agent and citric acid as a salivating agent, whichcomposition is cheaper to produce than known compositions according tothe pre-amble.

It is yet another object of the present invention to provide analternative composition, specifically a jelly, the use of whichcomposition as an auxiliary means is to ease the taking of oralmedication in solid form, which composition comprises iota-carrageenanas a jellifying agent and citric acid as a salivating agent, whichcomposition obviates any further disadvantages of known auxiliary means,specifically a jelly, the use of which composition as an auxiliary meansis to ease the taking of oral medication in solid form, whichcomposition comprises iota-carrageenan as a jellifying agent and citricacid as a salivating agent.

SUMMARY OF THE INVENTION

One or more of the above-stated objects are achieved with a compositionin the form of a jelly, comprising iota-carrageenan, citric acid andmaltodextrin. In this composition iota-carrageenan acts as a jellifyingagent and citric acid acts as a salivating agent.

One or more of the above-stated objects are achieved with a composition,specifically a jelly, the use of which composition as an auxiliary meansis to ease the taking of oral medication in solid form, whichcomposition comprises iota-carrageenan as a jellifying agent and citricacid as a salivating agent, characterized in one aspect of the inventionin that the composition further comprises maltodextrin. The relatedtechnical advantage is that addition of maltodextrin improves thecapability of the composition to keep the solid-form oral medicationsuspended when the latter is coated with the composition.

Preferably, the composition comprises maltodextrin in 1-4% in mass ofthe total mass of the composition. This offers the technical advantageof a sufficient long time before the solid-form oral medication willsettle in the mouth. In a particular embodiment, the compositioncomprises maltodextrin in the range of 1.3-1.8% in mass of the totalmass of the composition. Most preferably, the composition comprisesmaltodextrin in 1.5% in mass of the total mass of the composition. Thisoffers the advantage of an optimum settling time and hence allowsufficient time for even people with very strong aversions to swallowingto swallow the solid-form oral medication that is suspended in thecomposition in the mouth.

The publication NL-1039241 (D1) discloses a jelly comprising iotacarrageenan, citric acid and maltodextrin which is comprised in asalivating mix. The jelly can be used to coat solid medication before itis brought into the mouth. The jelly facilitates in taking oralmedication in solid form (page 5, line 1-page 7, line 21). Themaltodextrin comprised in the salivating mix is calculated to amount to1.14% in mass of the total mass of the composition.

The present invention signifies a selection invention over thedisclosure of D1, in particular in regard of the aspect of yield stress.The yield stress is the force or stress required to break down theviscosity of the composition, allowing solid medication to separate fromthe layer of (jelly) composition enclosing it. The higher the yieldstress, the more effective the (jelly) composition is in its describedfunction. Data of comparative tests are described later in relation toFIGS. 6-7. This data substantiates the technical advantages of theaddition of maltodextrin as mentioned in paragraph [0007] above (whichcorresponds to paragraph [0006] of patent application NL-2010552 fromwhich priority is claimed).

The present invention signifies that not only the viscosity of the jellycomposition is important, but that the visco-elastic behaviour thereofis important too. It is known from prior art that a carrageenan gelshows visco-elastic behaviour. However, what was not known until now wasthat polymer-like structures such as those of starch and starchderivatives such as maltodextrin influence the yield stress in a way asto unexpectedly increase the same.

According to another aspect of the invention, the composition comprisescitric acid in 0.05 to 0.10% in mass of the total mass of thecomposition. The related technical advantage is that the citric acidimparts a neutral to slightly acidic taste to the composition, whichrange of tastes are acceptable to most people using oral medication.

Preferably, the composition comprises citric acid in the range of0.05-0.1% in mass, and more preferably 0.06% in mass, of the total massof the composition. The related technical advantage is that the pH ofthe composition can be regulated to lie in the range of 4.8-6.5, morepreferably in the range of 5.0-6.0, and most preferably for the pH to be5.5.

According to yet another aspect of the invention, the compositioncomprises a calcium sequestrant. The related technical advantage is thatthis sequestrant aids in adjusting the pH of the composition. Anotherrelated technical advantage is that this sequestrant also aids inadjusting the Ca-ion activity in the composition. A certain amount ofCa-ion activity is beneficial in order to maintain a desired viscosityof the composition during its production and also during use thereof,i.e. in the mouth.

In and of itself the use of calcium in carrageenan jellies is known fromthe prior art. For example according to publication JP 2003/104912 (D2)calcium ions are used as a coagulation inhibitor (paragraph 0019). Thedisclosure relates to Ca²⁺-containing ionic matter in an amount of0.01-10 times (by weight) the amount of carrageenan in the composition.Also, it is disclosed in publication US 2007/128285 (D3) that theinclusion of water-soluble salts of metal ions such as a calcium orpotassium ion (e.g. the inorganic acid salts such as chloride, phosphateor of sulphuric acid, or organic acid salts such as of lactic acid orcitric acid) into the composition is effective in order to jellify thecomposition and enhance the jelly stability (paragraphs 0039-0042).

A calcium sequestrant provides calcium ions. While not intending to bebound by any theory, the inventor believes that the calcium ions, asindeed other divalent metal ions, strengthen the structure of the jellyclue to the calcium forming ionogenous bridges between carrageenanmolecules by way of its sulphate group. In addition to calcium chloride,other calcium sequestrants are, inter alia, calcium carbonate andcalcium oxide. Addition of calcium carbonate to a composition accordingto the invention will increase the pH, so a skilled person willcontemplate the addition of citric acid in order to lower the pH to adesirable value of 4.8-5.8. All alternatives will, of course, be subjectto compatibility with health regulations relating to the use of acomposition as an auxiliary means to ease the taking of oral medicationin solid form, and as such may require workshop modifications by askilled person.

The aspect of inclusion of a calcium sequestrant in a compositioncomprising iota-carrageenan, citric acid and maltodextrin according tothe invention signifies novelty and an inventive step over thedisclosures of D2 and D3 in light of the disclosure of D1. D2 disclosesthe use of calcium ions as a coagulation inhibitor and D3 discloses theuse of calcium ions as a jellifying agent. Inclusion of a calciumsequestrant affords a higher yield stress of the composition. The higherthe yield stress, the more effective the composition (jelly) is in itsdescribed function. Data of comparative tests with and without calciumchloride are described later in relation to FIGS. 8-9. This datasubstantiates the technical advantages of the inclusion of a calciumsequestrant as mentioned in paragraph [0014] above (which is the same asparagraph [0009] of application NL-2010552 from which priority isclaimed).

The composition comprises an amount of a calcium sequestrant such thatthe Ca-ion activity of the composition is <500 ppm. Preferably, thecomposition comprises an amount of a calcium sequestrant such that theCa-ion activity of the composition is between 10 ppm and 100 ppm. Morepreferably, the composition comprises an amount of a calcium sequestrantsuch that the Ca-ion activity of the composition is between 20 ppm and80 ppm.

Preferably, the calcium sequestrant comprised in the composition is asalt of citric acid. This is advantageous as the composition alreadyneeds to comprise citric acid in order to impart a neutral to slightlyacidic taste to the composition. The amount of citric acid required willbe as much as is needed to hold the pH between 4.8 and 5.8. In practice,the amount of citric acid to be added will be in the order of magnitudeof 0.05-0.1% in mass of the total mass of the composition. Withoutintending to be bound by any theory, the inventor offers the followingexplanation. During production of iota carrageenan, potassium hydroxideis used for adjusting the pH. Use of this iota carrageenan for thecomposition of the invention leads to ca. 3000 ppm of potassium beingcomprised in the composition. So upon addition of citric acid, in firstinstance potassium citrate will be formed and calcium will bond to thesulphate groups of the iota carrageenan until all potassium has bonded.It should clear that the use of iota carrageenan from a different sourcemay lead to a different amount of potassium, or an equivalent, beingcomprised in the composition, and to a slight variation in the amount ofcitric acid needed to hold the pH between 4.8 and 5.8.

Also preferably, and as an alternative, the calcium sequestrantcomprised in the composition is calcium chloride. This offers theadvantage of a readily available and cheaper alternative sequestrant.Preferably, the amount of calcium chloride comprised in the compositionis lower than 0.4% in mass relative to the total mass of thecomposition. More preferably, the amount of calcium chloride comprisedin the composition lies in the range of 0.0-0.2% in mass relative to thecomposition. Most preferably, the amount of calcium chloride comprisedin the composition is 0.005%-0.015% in mass relative to the total massof the composition. This offers the technical advantage of tailoring theshelf-life of the composition according to varying requirements.

DETAILED DESCRIPTION OF THE INVENTION

The composition according to the invention is qualified as universalbecause it can be used for the intake of any type of medication that canappropriately be taken orally. In particular, this composition is suitedfor facilitating the swallowing and oral administration of solid-formmedication, especially in the form of pills, tablets, capsules andpowders.

The composition according to the invention does not contain any activetherapeutic or prophylactic substance and thus can be used with allmedication in solid form, whatever the unitary form, dosage or activesubstance it might comprise.

According to one embodiment of the composition, it is provided in theform of a jellified paste that develops its lubricating properties whenit comes into contact with saliva and/or the mucosal membrane in themouth. These properties are enhanced by the presence of a salivatingagent. The composition according to the invention can be used tofacilitate the intake of medication, for example after mingling thecomposition and the medication on a spoon and bringing it into themouth. The medication can be used in its galenical, commercial form, asavailable in pharmacies. In practice, during the intake of medication,the composition takes the place of water which is generally used forswallowing capsules, pills, tablets or powders. The compositionaccording to the invention is in particular intended for people,especially children and elderly persons, who suffer frommedication-intake problems, and for people suffering from dysphasiaand/or xerostomia.

The composition according to the invention can be used to coatsolid-form medication, especially in the form of a tablet, pill, capsuleor powder, before it is brought into the mouth. No manipulation ormodification of the medication in the form of a tablet, pill, capsule orpowder is required. The tablet, pill, capsule or powder is simply placedin a sufficient quantity of composition, in order for the latter to coatthe former. The composition according to the invention is broughttogether with the medication in the form of a tablet, pill, capsule orpowder entirely in an intact form, without any modification of thismedication, such as through grinding of the pill or tablet, or openingof the capsule. Bringing the composition and the medication together canbe done by the patient himself, just before introducing the medicationinto the mouth. The pill, tablet, capsule or powder, in itscommercialized form, is taken up in the composition according to theinvention. Just before the intake, the medication in an independentunitary form is placed in the composition according to the invention,and then brought into the mouth. The medication in the form of a pill,tablet or capsule, can also be brought into the mouth in a separate way,before or after introducing the composition in the mouth. For example,it is possible to place the medication directly in the mouth and to takethe composition subsequently, in the same way as using water. Inparticular, no opening of capsules, or crushing of pills or tabletsrequired if the medication is incorporated in its intact form in thecomposition according to the invention, before or after introduction inthe mouth.

According to one embodiment of the invention, the composition comprisescitric acid. One of its functions is to act as a salivating agent.Another of its functions is to impart a neutral to slightly acidic tasteto the composition. Alternatively, one or several other compoundsstimulating saliva-production in the mouth can replace citric acideither entirely or in part to the extent of its amount in thecomposition. An example of an alternative is ascorbic acid.

According to a further embodiment, citric acid is comprised in thecomposition in an amount of 0.05-0.10% in mass, preferably 0.05-0.08% inmass and most preferably 0.06% in mass, relative to the total mass ofthe composition.

According to yet another embodiment, the composition comprises an amountof citric acid such as to obtain a pH that lies in the range of 4.8-6.5,preferably 5.0-6.0 and most preferably 5.5.

According to another embodiment, the composition comprisesiota-carrageenan in an amount of 0.5-2.0% in mass, preferably 0.7-1.0%in mass, relative to the total mass of the composition.

Carrageenans are linear sulphated polysaccharides that are oftenextracted from red seaweeds. It may be a carrageenan of the molecularstructure types α, β, γ, θ, λ, μ, σ, ν, ι, or κ. Carrageenans arecommercially available in the form of kappa (κ), iota (ι) or lambda (λ).In the present invention, the iota (ι) form is used. The iota form isoften derived from Eucheuma spinosum. An advantage of theiota-carrageenan is that it is thixotropic. The presence of thisjellifying agent imparts a naturally pleasant and appetizing characterto the composition while it also serves the function of lubricating theupper respiratory tract (mouth, pharynx and larynx) and subsequently theoesophagus. When the composition is present in the mouth and it is incontact with saliva, it immediately reacts as a lubricating substance.The presence of a salivating substance, especially on the basis ofcitric acid, induces hyper-salivation that further contributes to easeof swallowing.

It is possible to use another jellifying agent in combination with theiota-carrageenan. This jellifying agent can be another polysaccharide,for example cellulose or agar. The jellifying agent should be present insuch an amount in the composition that its mass percentage relative tothe total mass of carrageenan is less than 50%, preferably less than 30%and more preferably less than 10%, in order to prevent it from modifyingthe rheological properties of the composition. According to oneembodiment, iota-carrageenan is the only jellifying agent comprised inthe composition.

According to another embodiment, the composition has a certainvisco-elasticity. In particular, the measuring of the visco-elasticcomponents, storage G′ and loss G″ relative to the frequency ofdeformation of jellies according to the invention (measured, forexample, with a Rhéolab MCR 301 from Anton Paar at a constant amplitudeof 1% at 22° C.) shows that the storage modulus G′ is greater than theloss modulus G″. The relation between the two modules (G′ and G″)expressed as the formula tangent delta=G″/G′ is preferably always lessthan 1 for a range of frequencies between 0.1 and 100 s−1 equally.

In particular, the tangent delta is between 0.10 and 0.65. Moreover, thevalue of the tangent delta increases, in an advantageous manner relativeto the increase of the frequency. Such visco-elastic propertiesdetermine the formation of the composition as a stable elasticsubstance. These properties are obtained due to the presence ofiota-carrageenan in a sufficient amount.

DESCRIPTION OF THE DRAWINGS

The above and further preferred embodiments and technical advantages ofthe invention will now be described, by way of example, with referenceto the accompanying drawings in which:

FIGS. 1-5 depict the mechanical spectrum (values of G′ and G″ relativeto the frequency of deformation) of compositions that comprisesdifferent types of carrageenan in different amounts relative to thetotal mass of the composition.

FIGS. 6-7 depict the results of comparative tests of some compositionsaccording to the invention in regard of viscosity and the yield stress,respectively, as a function of the amount and the nature of maltodextrinpresent in the composition.

FIGS. 8-9 depict the results of comparative tests of some compositionsaccording to the invention in regard of viscosity and the yield stress,respectively, as a function of the amount and the nature of calciumpresent in the composition.

FIGS. 1-3 depict the mechanical spectrum (values of G′ and G″ relativeto the frequency of deformation) of compositions comprising varioustypes of carrageenan in an amount of 2% in mass relative to the totalmass of the composition. These Figures illustrate the differencesbetween the storage modulus G′ and the loss modulus G″ relative to thefrequency for the various compositions.

FIG. 1 relates to a composition comprising kappa-carrageenan. It revealsthat the storage modulus G′ is greater than the loss modulus, G″. Thedifference between G′ and G″ is not stable relative to the frequency,which means that the composition is very fragile.

FIG. 2 relates to a composition comprising lambda-carrageenan. Itreveals that there is no notable difference between the storage modulusG′ and the loss modulus G″. This is an expected outcome because thiscomposition does not jellify.

FIG. 3 relates to a composition comprising iota-carrageenan. It revealsthat the storage modulus G′ is much greater than the loss modulus G″.The difference between the two modules (G′ and G″) remains steady in thewhole range of frequencies, which means that there is a formation of acomposition with a stable elastic component.

FIG. 4 depicts the mechanical spectrum (values of G′ and G″ relative tothe frequency of deformation) of a composition comprisingiota-carrageenan in an amount of 0.7% in mass relative to the total massof the composition. It reveals a stable jellified condition even athigher frequencies.

FIG. 5 depicts the mechanical spectrum (values of G′ and G″ relative tothe frequency of deformation) of a composition comprisingiota-carrageenan in an amount of 0.5% in mass plus cellulose in anamount of 0.2% in mass, both relative to the total mass of thecomposition. It reveals that there is no jellified condition at higherfrequencies.

According to FIGS. 4 and 5, the composition comprising iota-carrageenanin an amount of 0.7% in relative mass has a tangent delta varying from0.6 to 0.17 and it thus provides a jellified structure at allfrequencies. For the composition comprising iota-carrageenan in anamount of 0.5% in relative mass and cellulose in an amount of 0.2% inrelative mass, the average tangent delta varies from 1.12 to 0.25, whichmeans that the composition provides a non-jellified structure at higherfrequencies. The addition of cellulose to a composition comprisingiota-carrageenan in an amount of 0.7% in relative mass does notguarantee a jellified structure at higher frequencies.

FIGS. 6 and 7 depict the results of comparative tests of somecompositions according to the invention in regard of viscosity and theyield stress, respectively, as a function of the amount and the natureof maltodextrin present in the composition.

The yield stress of the tested compositions was made through the use ofa controlled-stress rheometer, in this instance a Brookfield DX3TRVTRheometer. This type of instrument makes use of a controlled stress rampto gradually increase the amount of force on the sample until flow isinitiated. For this comparison the variable was the amount ofmaltodextrin in the composition. The composition comprised thefollowing:

-   -   water: balance    -   iota-carrageenan: 0.800%    -   aspartame: 0.055%    -   citric acid: 0.070%    -   maltodextrin: 0.00 to 2.00%    -   potassium sorbate: 0.800%    -   calcium chloride: 0.005%        The measurement results are:

% (mass) yield stress viscosity maltodextrin (Pa @ 20° C.) (mPa · s @20° C.) 0.0 10.6 14,560 0.5 40.4 11,660 1.0 42.1 12,300 1.1 42.3 12,6001.2 43.5 12,900 1.3 43.4 13,000 1.4 45.0 13,100 1.5 47.0 13,260 1.6 47.113,000 1.7 47.1 12,500 1.8 46.7 12,000 1.9 41.8 11,980 2.0 44.5 11,680

FIG. 6 shows the viscosity of a composition as a function of thepercentage (in mass) of maltodextrin in the composition. The viscosityis seen to have a clear build up around an optimum at 1.5%.

Measurement of the yield stress of the test compositions reveal asurprising relationship with the amount of maltodextrin in thecomposition. FIG. 7 shows that the yield stress increases with anincrease in the amount of maltodextrin, with an optimum in the range ofapprox. 1.3-1.8%.

In stark contrast, the composition of D1, comprising Salivating Mix(Firmenich) that in turn comprises maltodextrin in an amount calculatedto be approximately 1.14% by mass, has a yield stress of 5 Pa.

A possible explanation of a nearly eight-fold increase of the yieldstress of a composition according to the invention in comparison withthe yield stress of a composition according to D1 is as follows.Salivating Mix (Firmenich) comprises five components: two findingagents, citric acid, maltodextrin and modified starch. As shown in FIGS.6-7, a composition comprising carrageenan but no maltodextrin has alower yield stress than a composition comprising a certain amount ofmaltodextrin.

FIGS. 8 and 9 depict the results of comparative tests of somecompositions according to the invention in regard of viscosity and theyield stress, respectively, as a function of the amount and the natureof calcium present in the composition.

It was not known until now what effect, if any, calcium chloride has onthe yield stress of the composition. A series of compositions weretested, whereby the amount of maltodextrin was held at the optimum valueof 1.5% in mass (as based on results shown in FIGS. 6 and 7) and theamount of calcium chloride was varied between 0.0% and 2.0% in mass.

The composition comprised the following:

-   -   water: balance    -   iota-carrageenan: 0.800%    -   aspartame: 0.055%    -   citric acid: quantity sufficient to hold the pH at 4.8-5.8, in        practice ca. 0.05-0.1%    -   maltodextrin: 1.50%    -   potassium sorbate: 0.800%    -   calcium chloride: 0.0-2.0%        The measurement results are:

% (mass) yield stress viscosity calcium chloride (Pa @ 20° C.) (mPa · s@ 20° C.) 0.0 53 16,700 0.01 63 18,900 0.015 53 19,200 0.1 52 18,650 0.245 17,000 0.3 43 13,500 0.4 39 16,250In regard of both the viscosity and the yield stress an optimum isrevealed in the range of 0.0-0.4% in mass of calcium chloride. Mostpreferably, the amount of calcium chloride comprised in the compositionis 0.01% in mass relative to the total mass of the composition. Theresults are depicted in FIGS. 8-9.

A possible explanation of a relatively low viscosity of a compositioncomprising ca. 0.3% in mass of calcium chloride may lie in the formationof calcium citrate and there not being sufficient free calcium ions formatrix formation with electrostatic or ionic forces acting between thecarrageenan molecules. Reference is made to the explanation given abovethat upon addition of citric acid, in first instance potassium citratewill be formed and calcium will bond to the sulphate groups of the iotacarrageenan until all potassium has bonded The fact remains that withthe addition of calcium chloride according to the tested embodiments,the viscosity is at least the level of 12,000 mPa·s @ 20° C. with theabove-described surprising, approximately eight-fold increase in theyield stress of the composition (ca. 40 Pa or higher @ 20° C.) ascompared with the yield stress of a composition according to prior artD1 (5 Pa @ 20° C.).

Alternatives for calcium chloride as a calcium sequestrant are, interalia, calcium carbonate and calcium oxide. Addition of calcium carbonateto a composition according to the invention will increase the pH, so askilled person will contemplate the addition of citric acid in order tolower the pH to a desirable value in the range of 4.8-5.8. Allalternative calcium sequestrants will, of course, be subject tocompatibility with health regulations relating to the use of acomposition as an auxiliary means to ease the taking of oral medicationin solid form, and as such may require workshop modifications by askilled person.

DETAILED DESCRIPTION OF FURTHER EMBODIMENTS AND EXAMPLES

According to one aspect of the invention, a just balance needs to bestruck between the pourability of the composition and its viscosity. Itis presumed that in the throat of a person taking oral medication, thecomposition should flow easily but not so easily as to flow into theperson's wind-pipe. Therefore, it is desired that the composition has asuitable texture, not too short and not too long, so that when pouringthe composition it can just stop short of continuing as a thread.Additionally, it is desirable that the composition preferably has anon-sticky and otherwise only a very slight sticky mouth-feelconsidering that a composition sticking to the palate will inducerepeated swallows. Of course, the mouthfeel should not be more than justvery slightly sticky because repeated strong swallows after the firstswallow may cause discomfort, and may in certain circumstances even bedangerous, to some dysphagia patients.

During the course of producing and using the composition according tothe invention as an auxiliary means in easing the taking of oralmedication in solid form, it has been found that iota-carrageenanprovides for a stable viscous network that does not exhibit too stickyproperties, and that it provides for the most prolonged storagestability over time. Stability in the present context means that thecomposition does not show phase separation (e.g. aggregation, syneresisor precipitation). The absence of starch in the composition according tothe invention is an important feature considering that starch rendersthe composition sensitive to breakdown by amylase from the saliva ofdysphagia patients, thus decreasing the stability (of the viscosity) ofthe composition.

According to another aspect of the invention, phase separation, i.e. theformation of layers and changes in viscosity during storage of thecomposition are unwanted. A possible problem may lie in the formation ofcalcium-acid complexes, resulting in salt precipitates. To avoid suchproblems, calcium sequestrants, for example calcium chloride, or a saltof citric acid, are comprised in the composition in order to adjust thepH and also in order to adjust Ca-ion activity in the composition. Acertain amount of Ca-ion activity is beneficial in order to maintain adesired viscosity of the composition during its production and its lateruse. The presence of calcium ions helps the polymers in the compositionto re-arrange themselves around the calcium ions. The calcium ions alsoallow for a better orientation of the carrageenan molecules in thecomposition. Preferably, Ca-ion activity is between 10 ppm and 100 ppm,more preferably between 20 ppm and 80 ppm. To prevent the formation andprecipitation of insoluble calcium salts in time, calcium sequestrantsshould however be dosed with care. In general, the less the better, asevidenced by the results shown in FIG. 9. When calcium chloride is thecalcium sequestrant, the preferred amount thereof in the composition is0.005% in mass of the total mass of the composition.

A possible alternative solution to avoidance of phase separation of thecomposition of the invention lies in the use of anionic (water-)solublefibres. Anionic (water-) soluble fibres can bind calcium and thus aid inoptimizing the pH of the composition, and they can aid in increasing theviscosity of the composition. As such, examples of anionic(water-)soluble fibres are well known to the person skilled in the art.

According to an embodiment of the composition according to prior art D1,the composition comprises water in an amount of 80-99% in mass,preferably 84-97% in mass, relative to the total mass of thecomposition. The choice of the amount of water, in combination with thenature and the amount of iota-carrageenan, and optionally an amount ofan additional jellifying agent, allows for adjustment of the viscosityof the composition. The composition according to the invention has aviscosity of 500-4,500 mPa·s, and preferably 700-2,000 mPa·s, asmeasured with a Physica MC1 Rheometer from Anton Paar (measurement at 1min 20 rpm at 22° C.). It is pointed out that measurement of theviscosity of the embodiments mentioned in paragraphs [0046] and [0048]were done using a different type of rheometer (Brookfield DX3TRVT) andat a different temperature. For embodiments of the composition accordingto the invention, a target value for the viscosity is approx.6,000-10,000 mPa·s, and preferably higher, at 20° C. as measured using aBrookfield Rheometer (1 min spindle 4 at 20 rpm).

According to a further embodiment of the present invention, thecomposition comprises a preservating agent. Examples of a suitablepreservating agent are potassium sorbate and sodium benzoate.Preferably, the preservating agent is potassium sorbate, comprised in anamount of 0.2-1.0% in mass, more preferably comprised in an amount of0.4-0.8% in mass, and even more preferably in an amount of 0.6-0.8% inmass, relative to the total mass of the composition.

According to a further embodiment, the composition comprises aflavouring agent, preferably for orange, lemon, lime, red fruit (e.g.cherry and strawberry) or mint flavours. The flavouring agent iscomprised in an amount of 0.05-0.20% in mass, preferably in an amount of0.07-0.10% in mass, relative to the total mass of the composition.

According to a further embodiment, the composition comprises asweetening agent chosen from the group of: saccharose, aspartame,sucralose, stevia, inulin and derivatives thereof. For example, if thesweetening agent is saccharose, then it should be comprised in thecomposition in an amount of 15-20% in mass, preferably 12-13% in mass,relative to the total mass of the composition. If the sweetening agentis aspartame, then it should be comprised in the composition in anamount of 0.03-0.06% in mass relative to the total mass of thecomposition.

According to one specific embodiment, the composition according to theinvention comprises (all amounts in mass % relative to the total mass ofthe composition):

iota-carrageenan 0.5-2%, preferably 0.7-1.0% citric acid 0.05-0.10%,preferably 0.05-0.08% maltodextrin 1.0-2.0%, preferably 1.3-1.8%potassium sorbate 0.4-0.8%, preferably 0.6-0.8% saccharose 15-20%,preferably 12-13% flavouring agent 0.05-0.20%, preferably 0.07-0.10%water approximately 80-90%, for example 85%

According to another embodiment, the composition according to theinvention comprises (all amounts in mass % relative to the total mass ofthe composition):

iota-carrageenan 0.5-2.0%, preferably 0.7-1.0% citric acid 0.05-0.10%,preferably 0.05-0.08% maltodextrin 1.0-2.0%, preferably 1.3-1.8%potassium sorbate 0.4-0.8%, preferably 0.6 to 0.8% aspartame 0.03-0.06%flavouring agent 0.05-0.20%, preferably 0.07-0.10% water approximately95-99%, for example 98%

According to another embodiment, the composition according to theinvention is characterized by the absence of one or more ofhydroxypropyl methylcellulose, gelatin, spilanthol, jambu oleoresin andagar.

According to another embodiment, the composition according to theinvention is characterized by the absence of one or more of carob,carboxymethyl cellulose and xanthan gum.

BEST MODE OF THE INVENTION

A composition according to the invention can be prepared in a simpleway, by dissolving the iota-carrageen in water at a temperature ofaround 60° C. The other components to be comprised in the compositioncan be added during the formation of the composition when it is stillhot, or when the composition is at room temperature, this depending onthe heat-resistance and the solvability of such components in thecomposition.

A non-limitative example of production of the composition is givenbelow. The production steps are roughly as follows: Weigh the water andthe potassium sorbate in a beaker, then heat up to 60° C. while stirringwith a magnetic stirrer. If a colouring agent is required, then itshould be added at this stage. Next, weigh the jellifying agent in abeaker. When the water is at the right temperature and the potassiumsorbate has completely dissolved, place the beaker in a turbine andstart agitating at 700 rpm. Then add the jellifying agent to thecontents of the beaker and increase agitation to the rate of 1,500 rpm.Carry on agitating for 20 minutes. When the composition is back at roomtemperature, weigh the maltodextrin, the citric acid, and the calciumsequestrant and add these to the contents of the beaker. Continueagitating the contents and add any desired flavouring agent.

The present invention thus provides a composition, specifically a jelly,the use of which is to ease the taking of oral medication in solid form,and to the use of such a composition as an auxiliary means for thestated purpose. The invention relates in one aspect to a composition,specifically a jelly, the use of which composition as an auxiliary meansis to ease the taking of oral medication in solid form, whichcomposition comprises iota-carrageenan as a jellifying agent and citricacid as a salivating agent, characterized in that the compositionfurther comprises 1.3%-1.8% maltodextrin. In another aspect, thecomposition comprises a calcium sequestrant for adjusting Ca-ionactivity of the composition. In one embodiment, the compositioncomprises iota-carrageenan in 0.7-1.0% in mass, citric acid in 0.06% inmass, maltodextrin in 1.5% in mass, all relative to the total mass ofthe composition, and an amount of a calcium sequestrant such that theCa-ion activity of the composition is between 20 ppm and 80 ppm.

1. An oral composition in the form of a jelly to aid in the delivery ofa solid-form oral medication, wherein the oral composition comprises:(i) iota-carrageenan, (ii) citric acid, and (iii) maltodextrin, whereinthe oral composition comprises the iota-carrageenan and the citric acidin an amount within a range of 0.5-2.0 mass %, based on the total massof the oral composition so that the oral composition exhibits a yieldstress of 15 Pa or higher at 20° C. as measured using a BrookfieldDX3TRVT rheometer that makes use of a controlled-stress ramp togradually increase the amount of force on the sample until flow isinitiated.
 2. The oral composition according to claim 1, wherein themaltodextrin is added as a separate component to a nascent compositioncomprising the iota-carrageenan.
 3. The oral composition according toclaim 1, wherein hydroxypropyl methylcellulose, gelatin, spilanthol,jambu oleoresin, agar, carob, carboxy methylcellulose or xanthan gum arenot present in the composition.
 4. The composition according to claim 1,wherein the maltodextrin is present in the composition in an amount of1.3-1.8 mass %, based on the total mass of the composition.
 5. Thecomposition according to claim 1, wherein the citric acid is present inthe composition in an amount of 0.05 to 0.10 mass %, based on the totalmass of the composition.
 6. The composition according to claim 1,wherein the citric acid is present in the composition in an amountsufficient to achieve a pH of the composition within a range of 4.8 to6.5.
 7. The composition according to claim 1, wherein the compositionfurther comprises a calcium sequestrant in an amount sufficient toadjust Ca-ion activity of the composition to achieve a Ca-ion activityof the composition which is <500 ppm.
 8. The composition according toclaim 7, wherein the calcium sequestrant is calcium chloride.
 9. Thecomposition according to claim 7, wherein the calcium sequestrant iscalcium carbonate.
 10. The composition according to claim 8, wherein thecalcium chloride is present in the composition in an amount lower than0.4 mass %, based on the total mass of the composition.
 11. Thecomposition according to claim 1, wherein the iota-carrageenan ispresent in the composition in an amount of 0.5 to 2 mass %, based on thetotal mass of the composition.
 12. The composition according to claim 1,wherein the composition further comprises water in an amount of 80-99mass %, based on the total mass of the composition.
 13. The compositionaccording to claim 1, wherein the composition further comprises aflavouring agent that provides the composition with a flavor selectedfrom the group consisting of orange flavor, lemon flavor, lime flavor,red fruit flavor and mint flavor.
 14. The composition according to claim1, wherein the composition further comprises a sweetening agent selectedfrom the group consisting of saccharose, aspartame, sucralose, steviaand inuline.
 15. The composition according to claim 1, wherein thecomposition comprises 0.8 mass % of the iota-carrageenan, 0.06-0.07 mass% of the citric acid, 1.5 mass % of the maltodextrin and 0.005 mass % ofcalcium chloride, based on the total mass of the composition.
 16. Thecomposition according to claim 1, wherein the composition furthercomprises 0.005-0.4 mass % of calcium chloride, based on the total massof the composition.
 17. The composition according to claim 4, whereinthe maltodextrin in the composition is present in the composition in anamount of 1.5 mass %, based on the total mass of the composition. 18.The composition according to claim 5, wherein the citric acid is presentin the composition in an amount of 0.05 to 0.10 mass %, based on thetotal mass of the composition.
 19. The composition according to claim 6,wherein the citric acid is present in the composition in an amountsufficient to achieve a pH of the composition of 5.5.
 20. Thecomposition according to claim 7, wherein the calcium sequestrant ispresent in an amount sufficient to achieve a Ca-ion activity of thecomposition which is between 10 ppm and 100 ppm.
 21. The compositionaccording to claim 7, wherein the calcium sequestrant is present in anamount sufficient to achieve a Ca-ion activity of the composition whichis between 20 ppm and 80 ppm.
 22. The composition according to claim 10,wherein the calcium chloride is present in the composition in an amountof 0.005-0.015 mass %, based on the total mass of the composition. 23.The composition according to claim 11, wherein the iota-carrageenan ispresent in the composition comprised in an amount of 0.7 to 1.0 mass %,based on the total mass of the composition.
 24. The compositionaccording to claim 11, wherein the water is present in the compositionin an amount of 84-97 mass %, based on the total mass of thecomposition.
 25. The composition according to claim 16, wherein thecalcium chloride is present in an amount of 0.005-0.015 mass %, based onthe total mass of the composition.
 26. The composition according toclaim 1, wherein the composition comprises: (i) 1.5 mass % of themaltodextrin, (ii) 0.80 mass % of the iota-carrageenan, (iii) 0.055 mass% of aspartame, (iv) 0.070 mass % of the citric acid, (v) 0.80 mass % ofpotassium sorbate, and (vi) 0.00-0.40 mass % of calcium chloride. 27.The composition according to claim 1, wherein the composition comprises:(i) 0.5-2.0 mass % of the maltodextrin, (ii) 0.80 mass % of theiota-carrageenan, (iii) 0.055 mass % of aspartame, (iv) 0.070 mass % ofthe citric acid, (v) 0.80 mass % of potassium sorbate, and (vi) 0.005mass % of calcium chloride.
 28. A solid-form oral medication whichincludes a coating comprised of the composition according to claim 1.29. A method of making an oral composition in the form of a jelly to aidin the delivery of a solid-form oral medication, wherein the methodcomprises comprising the steps of: (a) forming a nascent compositioncomprising iota-carrageenan; and (b) adding maltodextrin as a separatecomponent to the nascent composition according to step (a) in an amountwithin a range of 0.5-2.0 mass %, based on the total weight of thecomposition so that the composition exhibits a yield stress of 15 Pa orhigher at 20° C. as measured using a Brookfield DX3TRVT rheometer thatmakes use of a controlled-stress ramp to gradually increase the amountof force on the sample until flow is initiated; and (c) adding citricacid to the nascent composition.
 30. The method according to claim 29,wherein hydroxypropyl methylcellulose, gelatin, spilanthol, jambuoleoresin, agar, carob, carboxy methylcellulose or xanthan gum are notpresent in the composition.
 31. An oral composition obtained by theprocess according to claim
 29. 32. An oral medication comprising theoral composition in the form of a jelly according to claim 1, and asolid-form oral medication coated by the jelly.